Surface functionalization is one of the key steps toward the utilization of mesoporous materials in drug delivery system. Here, the folic acid (FA) ligands are conjugated onto poly(ethylene imine) (PEI) modified SBA-15 particles (PEI/SBA-15) via amide reaction, which results in the FA/PEI/SBA-15 particles. Doxorubicin hydrochloride (DOX), an anticancer drug, is successfully loaded into these particles. The in vitro cytotoxicity and cellular uptake of the empty FA/PEI/SBA-15 particles and the DOX-loaded ones are evaluated on two kinds of cancer, cells (HeLa cells and A549 cells). Specifically, an excellent cellular uptake using the current anticancer drug delivery vehicles (DOX-loaded FA/PEI/SBA-15 particles) mediated by the FA receptor is demonstrated by fluorescence microscope and flow cytometry. The FA/PEI/SBA-15 particles demonstrate a lower cytotoxicity comparing with the PEI/SBA-15 particles, while the DOX-loaded FA/PEI/SBA-15 particles exhibit much greater inhibition to the studied cancer cells. Furthermore, the in vitro release study shows that the targeted FA/PEI/SBA-15 particles have a typical sustained release behavior. This work therefore demonstrates that drug-loaded FA/PEI/SBA-15 particles have great potential application in targeted anticancer drug delivery for cancer therapy. (C) 2012 Elsevier Inc. All rights reserved.